Category: 166196-54-9

Hansen, Joshua D. published the artcilePotent and selective pyrazole-based inhibitors of B-Raf kinase, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, the main research area is pyrazole derivative inhibitor B Raf kinase antitumor.

Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Lesniak, Robert K. published the artcileDiscovery of 1H-Pyrazole Biaryl Sulfonamides as Novel G2019S-LRRK2 Kinase Inhibitors, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, the main research area is pyrazole biaryl sulfonamides preparation G2019S LRRK2 kinase inhibitor.

G2019S (GS) is the most prevalent mutation in the leucine rich repeat protein kinase 2 gene (LRRK2), a genetic predisposition that is common for Parkinson’s disease, as well as for some forms of cancer, and is a shared risk allele for Crohn’s disease. GS-LRRK2 has a hyperactive kinase, and although numerous drug discovery programs have targeted LRRK2 kinase, few have reached clin. development. We report the discovery and preliminary development of an entirely novel structural class of potent and selective GS-LRRK2 kinase inhibitors: biaryl-1H-pyrazoles.

ACS Medicinal Chemistry Letters published new progress about Crohn disease. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Recommanded Product: 4-(4-Bromo-1H-pyrazol-3-yl)pyridine.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics

Khonde, Lutete Peguy published the artcile1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in Mycobacterium tuberculosis, Application In Synthesis of 166196-54-9, the main research area is diarylpyrazolyl acylsulfonamide preparation antituberculosis activity.

Phenotypic whole cell high-throughput screening of a ~150,000 diverse set of compounds against Mycobacterium tuberculosis (Mtb) in cholesterol-containing media identified 1,3-diarylpyrazolyl-acylsulfonamide I as a moderately active hit. Structure-activity relationship (SAR) studies demonstrated a clear scope to improve whole cell potency to MIC values of <0.5μM, and a plausible pharmacophore model was developed to describe the chem. space of active compounds Compounds are bactericidal in vitro against replicating Mtb and retained activity against multidrug-resistant clin. isolates. Initial biol. triage assays indicated cell wall biosynthesis as a plausible mode-of-action for the series. However, no cross-resistance with known cell wall targets such as MmpL3, DprE1, InhA, and EthA was detected, suggesting a potentially novel mode-of-action or inhibition. The in vitro and in vivo drug metabolism and pharmacokinetics profiles of several active compounds from the series were established leading to the identification of a compound for in vivo efficacy proof-of-concept studies. Journal of Medicinal Chemistry published new progress about Homo sapiens. 166196-54-9 belongs to class pyrazoles-derivatives, name is 4-(4-Bromo-1H-pyrazol-3-yl)pyridine, and the molecular formula is C8H6BrN3, Application In Synthesis of 166196-54-9.

Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics